PE20060374A1 - FUSED HETEROCYCLIC KINASE INHIBITORS - Google Patents

FUSED HETEROCYCLIC KINASE INHIBITORS

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Publication number
PE20060374A1
PE20060374A1 PE2005000752A PE2005000752A PE20060374A1 PE 20060374 A1 PE20060374 A1 PE 20060374A1 PE 2005000752 A PE2005000752 A PE 2005000752A PE 2005000752 A PE2005000752 A PE 2005000752A PE 20060374 A1 PE20060374 A1 PE 20060374A1
Authority
PE
Peru
Prior art keywords
iloxi
triazin
fluorophenyl
thiourea
methoxy
Prior art date
Application number
PE2005000752A
Other languages
Spanish (es)
Inventor
Robert M Borzilleri
Zhong Chen
Tram N Huynh
Xiao Tao Chen
Zhen-Wei Cai
Kyoung S Kim
Wayne Vaccaro
Original Assignee
Bristol Myers Squibb Co
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Publication date
Application filed by Bristol Myers Squibb Co filed Critical Bristol Myers Squibb Co
Publication of PE20060374A1 publication Critical patent/PE20060374A1/en

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/53Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with three nitrogens as the only ring hetero atoms, e.g. chlorazanil, melamine
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/04Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/16Drugs for disorders of the alimentary tract or the digestive system for liver or gallbladder disorders, e.g. hepatoprotective agents, cholagogues, litholytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/08Drugs for disorders of the urinary system of the prostate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P13/00Drugs for disorders of the urinary system
    • A61P13/12Drugs for disorders of the urinary system of the kidneys
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    • A61P17/00Drugs for dermatological disorders
    • A61P17/06Antipsoriatics
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P19/00Drugs for skeletal disorders
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/02Drugs for skeletal disorders for joint disorders, e.g. arthritis, arthrosis
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    • A61P19/00Drugs for skeletal disorders
    • A61P19/08Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease
    • A61P19/10Drugs for skeletal disorders for bone diseases, e.g. rachitism, Paget's disease for osteoporosis
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    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/14Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
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    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
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    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
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    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
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    • A61P35/00Antineoplastic agents
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    • A61P37/00Drugs for immunological or allergic disorders
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    • A61P37/00Drugs for immunological or allergic disorders
    • A61P37/02Immunomodulators
    • A61P37/06Immunosuppressants, e.g. drugs for graft rejection
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • A61P7/06Antianaemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/06Antiarrhythmics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D473/00Heterocyclic compounds containing purine ring systems
    • C07D473/26Heterocyclic compounds containing purine ring systems with an oxygen, sulphur, or nitrogen atom directly attached in position 2 or 6, but not in both
    • C07D473/28Oxygen atom
    • C07D473/30Oxygen atom attached in position 6, e.g. hypoxanthine
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D495/00Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04Ortho-condensed systems

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  • Engineering & Computer Science (AREA)
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  • Diabetes (AREA)
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  • Rheumatology (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Heart & Thoracic Surgery (AREA)
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  • Pain & Pain Management (AREA)
  • Endocrinology (AREA)
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  • Ophthalmology & Optometry (AREA)
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Abstract

SE REFIERE A UN COMPUESTO DE FORMULA I O II, DONDE R1 ES H, ALQUILO, CICLOALQUILO, FENILO, FLUOROFENILO, ENTRE OTROS; R2 ES H, HALOGENO, CIANO, NO2, ENTRE OTROS; B ES O, S, SO, ENTRE OTROS; V ES CH2, NH, ENTRE OTROS; W, X SON CADA UNO C, N; Y ES O, S, NH, N-HALOGENO; ENTRE OTROS; Z ES NH, CH2, ENTRE OTROS; n ES 0-4; A ES 6-METOXI-5-METIPIRROLO[2,1-f][1,2,4]TRIAZIN-4-ILOXI, 6-CLORO-1-METIL-1H-PIRAZOLO[3,4-d]PIRIMIDIN-4-ILOXI, 5-METILPIRROLO[2,1-f][1,2,4]TRIAZIN-6-CARBOXILATO, ENTRE OTROS. SON COMPUESTOS PREFERIDOS: 1-(3-FLUORO-4-(6-METOXI-5-METILPIRROLO[2,1-f][1,2,4]TRIAZIN-4-ILOXI)FENIL)-3-(2-FENILACETIL)TIOUREA; 1-(3-FLUORO-4-(6-METOXI-5-METILPIRROLO[2,1-f][1,2,4]TRIAZIN-4-ILOXI)FENIL)-3-(2-(4-FLUOROFENIL)ACETIL)TIOUREA; 1-(4-(6-CLORO-1-METIL-1H-PIRAZOLO[3,4-d]PIRIMIDIN-4-ILOXI)-3-FLUOROFENIL)-3-(2-(4-FLUOROFENIL)ACETIL)TIOUREA, ENTRE OTROS. SE REFIERE TAMBIEN A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON INHIBIDORES DE LA ACTIVIDAD TIROSINA CINASA DE LOS RECEPTORES DEL FACTOR DE CRECIMIENTO TALES COMO C-MET, UTILES EN EL TRATAMIENTO DEL CANCERREFERS TO A COMPOUND OF FORMULA I OR II, WHERE R1 IS H, ALKYL, CYCLOALKYL, PHENYL, FLUOROPHENYL, AMONG OTHERS; R2 IS H, HALOGEN, CYANE, NO2, AMONG OTHERS; B IS O, S, SO, AMONG OTHERS; V IS CH2, NH, AMONG OTHERS; W, X ARE EACH C, N; Y IS O, S, NH, N-HALOGEN; AMONG OTHERS; Z IS NH, CH2, AMONG OTHERS; n IS 0-4; A ES 6-METHOXY-5-METHYROLO [2,1-f] [1,2,4] TRIAZIN-4-ILOXI, 6-CHLORO-1-METHYL-1H-PYRAZOLO [3,4-d] PYRIMIDIN-4 -YLOXY, 5-METHYLPYRROL [2,1-f] [1,2,4] TRIAZIN-6-CARBOXYLATE, AMONG OTHERS. PREFERRED COMPOUNDS ARE: 1- (3-FLUORO-4- (6-METHOXY-5-METHYLPYRROL [2,1-f] [1,2,4] TRIAZIN-4-ILOXI) PHENYL) -3- (2-PHENYLACETILE ) THIOUREA; 1- (3-FLUORO-4- (6-METHOXY-5-METHYLPYRROLO [2,1-f] [1,2,4] TRIAZIN-4-ILOXI) PHENYL) -3- (2- (4-FLUOROPHENYL) ACETYL) THIOUREA; 1- (4- (6-CHLORO-1-METHYL-1H-PYRAZOLO [3,4-d] PYRIMIDIN-4-ILOXI) -3-FLUOROPHENYL) -3- (2- (4-FLUOROPHENYL) ACETYL) THIOUREA, AMONG OTHERS. IT ALSO REFERS TO A PHARMACEUTICAL COMPOSITION. SUCH COMPOUNDS ARE INHIBITORS OF THE TIROSINE KINASE ACTIVITY OF GROWTH FACTOR RECEPTORS SUCH AS C-MET, USEFUL IN THE TREATMENT OF CANCER

PE2005000752A 2004-06-28 2005-06-28 FUSED HETEROCYCLIC KINASE INHIBITORS PE20060374A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US58345904P 2004-06-28 2004-06-28
US61256304P 2004-09-23 2004-09-23

Publications (1)

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PE20060374A1 true PE20060374A1 (en) 2006-05-07

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ID=35457856

Family Applications (2)

Application Number Title Priority Date Filing Date
PE2005000754A PE20060524A1 (en) 2004-06-28 2005-06-28 HETEROCICLIC FUSED COMPOUNDS AS INTERMEDIARIES IN THE PREPARATION OF KINASE INHIBITING PYRROLOTRIAZINES
PE2005000752A PE20060374A1 (en) 2004-06-28 2005-06-28 FUSED HETEROCYCLIC KINASE INHIBITORS

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PE2005000754A PE20060524A1 (en) 2004-06-28 2005-06-28 HETEROCICLIC FUSED COMPOUNDS AS INTERMEDIARIES IN THE PREPARATION OF KINASE INHIBITING PYRROLOTRIAZINES

Country Status (14)

Country Link
US (2) US20050288290A1 (en)
EP (3) EP1771177A4 (en)
JP (3) JP4782117B2 (en)
KR (3) KR20070026621A (en)
AR (2) AR050254A1 (en)
AU (2) AU2005259894C1 (en)
BR (1) BRPI0512722A (en)
CA (1) CA2571680A1 (en)
IL (1) IL180325A0 (en)
MX (2) MXPA06015032A (en)
NO (3) NO20070453L (en)
PE (2) PE20060524A1 (en)
TW (2) TW200604184A (en)
WO (3) WO2006004636A2 (en)

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